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SML3692

Sigma-Aldrich

SSR149415

≥98% (HPLC)

Sinonimo/i:

(-)-(2S,4R)-1-[5-Chloro-1-[(2,4-dimethoxyphenyl)sulphonyl]-3-(2-methoxyphenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine-carboxamide, (2S,4R)-1-[(3R)-5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-(2-methoxyphenyl)-2-oxo-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidinecarboxamide, Nelivaptan, SSR 149415, SSR-149415

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About This Item

Formula empirica (notazione di Hill):
C30H32ClN3O8S
Numero CAS:
439687-69-1
Peso molecolare:
630.11
Numero MDL:
MFCD06199090
Codice UNSPSC:
51111800
Codice UNSPSC:
12352200
NACRES:
NA.21

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

-10 to -25°C

Azioni biochim/fisiol

SSR149415 is an orally active, selective vasopressin V1b receptor antagonist (human/rat Ki in nM = 1.5/1.3/V1b, 91/1050/V1a, 1412/2897/V2, 174/270/OT) that inhibits 30 nM AVP-induced Ca2+ response in human and rat V1b CHO transfectants (Ki = 1.26/2.0 nM). SSR149415 suppresses AVP-mediated physiological responses in vivo, including corticotropin secretion (1-30 mg/kg p.o. or i.p. in rats) upon exogenous AVP administration (0.3 µg/kg alone or 0.03 µg/kg with 0.1 µg corticoliberin/kg via i.v.), restraint stress-Induced corticotropin secretion (EC50 = 10 mg/kg i.p. in rats), and in a murine model of anxiety (four-plate test; 1-10 mg/kg i.p. or 3-10 mg/kg p.o. acute or 10 mg/kg/day p.o.).

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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The role of the vasopressin system and dopamine D1 receptors in the effects of social housing condition on morphine reward
Drug and Alcohol Dependence, 188, 113-118 (2018)
Identification of avian vasotocin receptor subtype-specific antagonists involved in the stress response of the chicken, Gallus gallus
Journal of Biomolecular Structure & Dynamics, 37(7), 1685-1699 (2019)
Differential activation of arginine-vasopressin receptor subtypes in the amygdaloid modulation of anxiety in the rat by arginine-vasopressin
Psychopharmacology, 235(4), 1015-1027 (2018)
V1b Receptor Antagonist SSR149415 and Naltrexone Synergistically Decrease Excessive Alcohol Drinking in Male and Female Mice
Alcohol, clinical & experimental research, 42(1), 195-205 (2018)
Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist
Journal of Pharmacology and Experimental Therapeutics, 300(3), 1122-1130 (2002)
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